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. 2003:1:e004.
doi: 10.1621/nrs.01004. Epub 2003 Jun 15.

Structural insights into regulation of nuclear receptors by ligands

Eric H Xu  1 , Millard H Lambert
Affiliations

Structural insights into regulation of nuclear receptors by ligands

Eric H Xu et al. Nucl Recept Signal. 2003.

Abstract

Nuclear receptors are DNA-binding transcription factors, the transcriptional function of many of which depends on the binding of ligands, a feature that distinguishes nuclear receptors from other transcription factors. This review will summarize recent advances in our knowledge of the interaction between selected nuclear receptors and their cognate ligands.

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Figures

Figure 1
Figure 1. Structural views of ligand-mediated recruitment of coactivators and corepressors to nuclear receptors.
A, structure of the PPAR α LBD bound to GW409544 and a SRC-1 coactivator motif (gold); B, structure of the PPAR α LBD bound to GW6471 and a SMRT corepressor motif (yellow); C, chemical structures of PPAR α agonist GW509544 and antagonist GW6471, D, comparison of corepressor and coactivator peptides bound to PPAR α.
Figure 2
Figure 2. Conservation of coactivator and corepressor binding pockets in nuclear receptors.
The residues that contact the SMRT corepressor motif are noted with arrows.
See this image and copyright information in PMC

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